› 4wbo

X-ray diffraction
2.81Å resolution

Bovine G Protein Coupled Receptor Kinase 1 in Complex with Amlexanox

Released:
DOI: 10.2210/pdb4wbo/pdb
PDB entry 4wbo coloured by chain, front view.
PDB entry 4wbo coloured by chain, side view.
PDB entry 4wbo coloured by chain, top view.
Source organism: Bos taurus
Primary publication:
Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor.
Homan KT, Wu E, Cannavo A, Koch WJ, Tesmer JJ
Molecules 19 16937-49 (2014)
PMID: 25340299

Function and Biology Details

Reaction catalysed: 
ATP + [rhodopsin] = ADP + [rhodopsin] phosphate
Biochemical function:
Biological process:
Cellular component:
Sequence domains:

Structure analysis Details

Assembly composition:
monomeric (preferred)
Assembly name:
PDBe Complex ID:
PDB-CPX-151205 (preferred)
Entry contents:
1 distinct polypeptide molecule
Macromolecule:
Rhodopsin kinase GRK1 Chains: A, B, C, D
Molecule details ›
Chains: A, B, C, D
Length: 541 amino acids
Theoretical weight: 61.22 KDa
Source organism: Bos taurus
Expression system: Trichoplusia ni
UniProt:
  • Canonical: P28327 (Residues: 1-535; Coverage: 95%)
Gene names: GRK1, RHOK
Sequence domains:
Structure domains:

Ligands and Environments

2 bound ligands:
Ligand ANW 4 x ANW
Ligand CL 4 x CL
No modified residues

Experiments and Validation Details

Entry percentile scores
X-ray source: APS BEAMLINE 21-ID-G
Spacegroup: P212121
Unit cell:
a: 118.112Å b: 119.166Å c: 174.261Å
α: 90° β: 90° γ: 90°
R-values:
R R work R free
0.243 0.241 0.267
Expression system: Trichoplusia ni

Quick links

Citations

7 review citations

The expanding GRK interactome: Implications in cardiovascular disease and potential for therapeutic development.
Hullmann et al. (2016)
6 more

1 mention without citation

Identification and characterization of amlexanox as a G protein-coupled receptor kinase 5 inhibitor.
Homan et al. (2014)